Cationic pentaheteroaryls as selective G-quadruplex ligands by solvent-free microwave-assisted synthesis

Petenzi M.; Verga D.; Largy E.; Hamon F.; Doria F.; Teulade-Fichou M.-P.; Guédin A.; Mergny J.-L.; Mella M.; Freccero M.

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Cationic pentaheteroaryls as selective G-quadruplex ligands by solvent-free microwave-assisted synthesis

机译：无溶剂微波辅助合成阳离子五杂芳基作为选择性G-四链体配体

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We report herein a solvent-free and microwaved-assisted synthesis of several water soluble acyclic pentaheteroaryls containing 1,2,4-oxadiazole moieties (1-7). Their binding interactions with DNA quadruplex structures were thoroughly investigated by FRET melting, fluorescent intercalator displacement assay (G4-FID) and CD spectroscopy. Among the G-quadruplexes considered, attention was focused on telomeric repeats together with the proto-oncogenic c-kit sequences and the c-myc oncogene promoter. Compound 1, and to a lesser extent 2 and 5, preferentially stabilise an antiparallel structure of the telomeric DNA motif, and exhibit an opposite binding behaviour to structurally related polyoxazole (TOxaPy), and do not bind duplex DNA. The efficiency and selectivity of the binding process was remarkably controlled by the structure of the solubilising moieties.

机译：我们在此报告了一种无溶剂的微波辅助合成方法，该方法合成了几种含有1,2,4-恶二唑基团（1-7）的水溶性无环戊杂芳基。通过FRET熔解，荧光嵌入剂置换试验（G4-FID）和CD光谱研究了它们与DNA四链体结构的结合相互作用。在所考虑的G-四链体中，注意力集中在端粒重复，原癌基因c-kit序列和c-myc癌基因启动子上。化合物1和较小程度的化合物2和5优先稳定端粒DNA基序的反平行结构，并表现出与结构相关的聚恶唑（TOxaPy）相反的结合行为，并且不结合双链体DNA。结合过程的效率和选择性由增溶部分的结构显着控制。

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《Chemistry: A European journal》 |2012年第45期|共10页
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Petenzi M.; Verga D.; Largy E.; Hamon F.; Doria F.; Teulade-Fichou M.-P.; Guédin A.; Mergny J.-L.; Mella M.; Freccero M.;
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正文语种 eng
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1; 2; 4-oxadiazoles; DNA recognition; G-quadruplexes; microwave chemistry; pentaheteroaryls;

机译：1;2;4-恶二唑;DNA识别;G-四链体;微波化学;五杂芳基;

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1. Cationic pentaheteroaryls as selective G-quadruplex ligands by solvent-free microwave-assisted synthesis [J] . Petenzi M., Verga D., Largy E., Chemistry: A European journal . 2012,第45期

机译：无溶剂微波辅助合成阳离子五杂芳基作为选择性G-四链体配体
2. Microwave-Assisted Synthesis of Arene Ru(II) Complexes Induce Tumor Cell Apoptosis Through Selectively Binding and Stabilizing bcl -2 G-Quadruplex DNA [J] . Yanhua Chen, Qiong Wu, Xicheng Wang, Materials . 2016,第5期

机译：芳烯ru（ii）络合物的微波辅助合成通过选择性结合和稳定Bcl -2 g-quadreplex DNA诱导肿瘤细胞凋亡
3. Designer ligands. VIII. thermal and microwave-assisted synthesis of silver(I)-selective ligands [J] . Andre Daubinet, Perry T.Kaye Synthetic Communications . 2002,第20期

机译：设计配体。八。热和微波辅助合成银（I）-选择性配体
4. Multistep Microwave-Assisted Solvent-Free Organic Reactions: Synthesis of 1,6-Disubstituted-4-Oxo-1,4-Dihydro-Pyridine-3-Carboxylic Acid Benzyl Esters [C] . Mauro Panunzio, Maria Antonietta Lentini, Eileen Campana, International Conference on Microwave and High Frequency Heating . 2006

机译：多步微波辅助溶剂有机反应：1,6-二取代-4-氧代-1,4-二氢 - 吡啶-3-羧酸苄基酯的合成
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

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6. Microwave-Assisted Synthesis of Arene Ru(II) Complexes Induce Tumor Cell Apoptosis Through Selectively Binding and Stabilizing bcl-2 G-Quadruplex DNA [O] . Yanhua Chen, Qiong Wu, Xicheng Wang, 2016

机译：微波辅助合成Arene Ru（II）配合物通过选择性结合和稳定bcl-2 G-Quadruplex DNA诱导肿瘤细胞凋亡。
7. Microwave-Assisted Synthesis of Arene Ru(II) Complexes Induce Tumor Cell Apoptosis Through Selectively Binding and Stabilizing bcl-2 G-Quadruplex DNA [O] . Yanhua Chen, Qiong Wu, Xicheng Wang, 2016

机译：微波辅助合成芳烃Ru（II）配合物通过选择性结合和稳定bcl-2 G-Quadruplex DNa诱导肿瘤细胞凋亡

Cationic pentaheteroaryls as selective G-quadruplex ligands by solvent-free microwave-assisted synthesis

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